2-Amidino analogs of glycine–amiloride conjugates: Inhibitors of urokinase-type plasminogen activator

…, WR Harley, NR Pasupuleti, FA Gorin, MH Nantz

Index: Massey, Archna P.; Harley, William R.; Pasupuleti, Nagarekha; Gorin, Fredric A.; Nantz, Michael H. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2635 - 2639

Full Text: HTML

Citation Number: 3

Abstract

The relative non-toxicity of the diuretic amiloride, coupled with its selective inhibition of the protease urokinase plasminogen activator (uPA), makes this compound class attractive for structure–activity studies. Herein we substituted the C (2)-acylguanidine of C (5)-glycyl- amiloride with amidine and amidoxime groups. The data show the importance of maintaining C (5)-hydrophobicity. The C (5)-benzylglycine analogs containing either C (2) ...